nvestigation of Chloroquine Resinate Feasibility and In Vitro Taste Masking Evaluation for Pediatric Formulation

Autor(es)

Guimaraes, Thiago F. ^[1] ; Vital, Italo Carlos F. ^[1] ; de Sousa, Eduardo G. R. ^[2] ; Boniatti, Janine ^[1] ; Bandini, Thiago B. ^[3] ; Carr, Olivia ^[4] ; Oliveira Jr, Osvaldo N. ; Shimizu, Flavio M. ^[5] ; da Fonseca, Lais B. ^[6] ; Vicosa, Alessandra L. ^[1]

Afiliação do(s) autor(es)

^[1] Fiocruz MS, Lab Farmacotecn Expt, Inst Tecnol Farmacos Famanguinhos, Rua Sizenando Nabuco 100, Rio De Janeiro, RJ - Brazil

^[2] Fiocruz MS, Inst Tecnol Farmacos Farmanguinhos, Secao Analise & Identificacao Compostos Com Poten, Rio De Janeiro, RJ - Brazil

^[3] Fiocruz MS, Inst Carlos Chagas ICC, Plataforma Espectrometria Massas, Curitiba, De De - Brazil

^[4] Univ Sao Paulo, Sao Carlos Inst Phys, POB 369, BR-13560970 Sao Carlos, SP - Brazil

^[5] Univ Campinas UNICAMP, Gleb Wataghin Inst Phys IFGW, Dept Appl Phys, BR-13083859 Campinas, SP - Brazil

^[6] Fiocruz MS, Serv Equivalencia & Farmacocinet, Rio De Janeiro, RJ - Brazil

• Tipo de documento: Artigo Científico
• Fonte: AAPS PHARMSCITECH; v. 23, n. 2 FEB 2 2022.
• Citações Web of Science: 0

Resumo

In this study, chloroquine resinates were prepared at a 1:1 (w:w) drug-to-resin ratio using the batch method with polacrilex (PC), sodium polystyrene sulfonate (SPS), and polacrilin potassium (PP) ion exchange resins (IER). The influence of drug/resin ratio and pH of the medium on drug loading efficiency was explored. UV-VIS spectrophotometric analysis showed that SPS resin had high loading efficiency for chloroquine diphosphate (CLP), above 89%, regardless of the pH. PP resin was more effective at pH 5.0 (90.68%) than at pH 1.0 (2.09%), and PC resin had only 27.63% of CLP loading efficiency. CLP complexation with IER yielded amorphous mixtures according to results from differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD), thus indicating drug-resin interaction. The taste masking efficiency was evaluated with in vitro methods using an adapted dissolution test and an electronic tongue system. During dissolution tests, SPS released only 1.0% of CLP after 300 s, while PP released over 10% after 90 s in simulated saliva solution. The electronic tongue distinguished the samples containing CLP, resins, and resinates by using multidimensional projection techniques that indicated an effective drug taste masking. In an accelerated stability study, the drug contents did not decrease in chloroquine resinates, and there was no physical degradation of the resinates after 60 days. Using chloroquine resinates therefore represents a novel way to evaluate taste masking in vitro which is relevant for the early formulation development process. (AU)

• Processo FAPESP: 18/22214-6 - Rumo à convergência de tecnologias: de sensores e biossensores à visualização de informação e aprendizado de máquina para análise de dados em diagnóstico clínico
• Beneficiário: Osvaldo Novais de Oliveira Junior
• Modalidade de apoio: Auxílio à Pesquisa - Temático